114150-50-4Relevant articles and documents
Targeted Detection of Cyclooxygenase-1 in Ovarian Cancer
Malerba, Paola,Crews, Brenda C.,Ghebreselasie, Kebreab,Daniel, Cristina K.,Jashim, Elma,Aleem, Ansari M.,Salam, Redoan A.,Marnett, Lawrence J.,Uddin, Md. Jashim
, p. 1837 - 1842 (2020)
Overexpression of cyclooxygenase-1 (COX-1) is associated with the initiation and progression of ovarian cancer, and targeted imaging of COX-1 is a promising strategy for early detection of this disease. We report the discovery of N-[(5-carboxy-X-rhodaminy
Synthesis of 1,5-diarylpyrazol-3-propanoic acids towards inhibition of cyclooxygenase-1/2 activity and 5-lipoxygenase-mediated LTB4 formation
Erguen, Burcu Caliskan,Nunez, Maria Teresa,Labeaga, Luis,Ledo, Francisco,Darlington, Janice,Bain, Gretchen,Cakir, Bilge,Banoglu, Erden
scheme or table, p. 497 - 505 (2011/05/09)
A set of 25 derivatives of 3-[1-(6-substituted-pyridazin-3-yl)-5-(4- substitutedphenyl)-1H-pyrazol-3-yl]propanoic acids has been synthesized and evaluated for their in vitro cyclooxygenase-1/2 (COX-1/ 2) inhibitory activity using assays with purified COX-1 and COX-2 enzymes as well as for their 5-lipoxygenase (5-LO)-mediated LTB4 formation inhibitory activity using an assay with activated human polymorphonuclear leukocytes (PMNL). Among the synthesized compounds, especially 4g showed COX-1 (IC50 = 1.5 μM) and COX-2 (IC50 = 1.6 μM) inhibitory activity, whereas compounds 4b and 4 f resulted in the inhibition of 5-LO-mediated LTB4 formation at 14 μM and 12 μM IC50 values, respectively, without any significant inhibition on COX isoforms. ECV · Editio Cantor Verlag.